AtorvaSTATin 是一种具有口服活性的 HMG-CoA 还原酶抑制剂,是一种降脂剂。它抑制人 SV-SMC 细胞的增殖和侵袭,IC50值分别为 0.39 μM 和 2.39 μM。
产品描述
Atorvastatin is an orally active inhibitor of HMG-CoA reductase,is a lipid-lowering agent (human SV-SMC proliferation and invasion with IC50s of 0.39 μM and 2.39 μM, respectively)
体外活性
In the atorvastatin group, myocardial cells were lined up more orderly and myocardial fibrosis level was decreased compared to the model group. The expressions of GRP78, caspase-12 and CHOP in myocardial cells were decreased in atorvastatin group. Moreover, in the atorvastatin-treated group the cell apoptosis rate was reduced and the endoplasmic reticulum (ER) stress was activated in response to heart failure and angiotensin II (Ang II) stimulation[1]
体内活性
Higher dose of atorvastatin can effectively suppress the development and progression of AAA induced by Ang II or CaCl2. Mechanistically, the activation of ER stress and inflammatory response were found involved in Ang II-induced AAA formation. The atorvastatin infusion significantly reduced ER stress signaling proteins, the number of apoptotic cells, and the activation of Caspase12 and Bax in the Ang II-induced ApoE-/- mice, compared with mice treated by Ang II alone. Furthermore, proinflammatory cytokines such as IL-6, IL-8, IL-1β were all remarkably inhibited after atorvastatin treatment. In vitro, the inhibitory effect of simvastatin on the ER stress signal pathway could be observed in both vascular smooth muscle cells and macrophages, and these inhibitory effects of statin were in a dose-dependent manner. In addition, apoptosis was induced with Ang II treatment. The maximal inhibitory effect of simvastatin on apoptosis was observed at 10 μmol/l.
Cas No.
134523-00-5
分子式
C33H35FN2O5
分子量
558.64
别名
阿伐他汀;阿托伐他汀
储存和溶解度
DMSO:80 mg/ml (143.20mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years